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https://www.readbyqxmd.com/read/28646346/adenosine-and-sleep
#1
Michael Lazarus, Jiang-Fan Chen, Zhi-Li Huang, Yoshihiro Urade, Bertil B Fredholm
The classic endogenous somnogen adenosine promotes sleep via A1 and A2A receptors. In this chapter, we present an overview of the current knowledge regarding the regulation of adenosine levels, adenosine receptors, and available pharmacologic and genetic tools to manipulate the adenosine system. This is followed by a summary of current knowledge of the role of adenosine and its receptors in the regulation of sleep and wakefulness. Despite strong data implicating numerous brain areas, including the basal forebrain, the tuberomammillary nucleus, the lateral hypothalamus, and the nucleus accumbens, in the adenosinergic control of sleep, the complete neural circuitry in the brain involved in the sleep-promoting effects of adenosine remains unclear...
June 24, 2017: Handbook of Experimental Pharmacology
https://www.readbyqxmd.com/read/28643232/caffeine-protects-against-anticonvulsant-induced-neurotoxicity-in-the-developing-rat-brain
#2
Stefanie Endesfelder, Ulrike Weichelt, Cornelia Schiller, Marco Sifringer, Ivo Bendix, Christoph Bührer
Phenobarbital is the most commonly used drug for the treatment of neonatal seizures but may induce neurodegeneration in the developing brain. Methylxanthine caffeine is used for the treatment of apnea in newborn infants and appears to be neuroprotective, as shown by antiapoptotic and anti-inflammatory effects in oxidative stress models in newborn rodents and reduced rates of cerebral palsy in human infants treated with caffeine. We hypothesized that caffeine may counteract the proapoptotic effects of phenobarbital in newborn rats...
June 22, 2017: Neurotoxicity Research
https://www.readbyqxmd.com/read/28611421/presence-of-caffeine-reversibly-interferes-with-efficacy-of-acupuncture-induced-analgesia
#3
Takumi Fujita, Changyong Feng, Takahiro Takano
Acupuncture is an alternative treatment for wide spectrum chronic pain. However, its validity remains controversial due to the disputed efficacy assessed in various clinical studies. Moreover, variability amongst individuals complicates the predictability of outcome, which impedes the integration of acupuncture into mainstream pain management programs. In light of our previous finding that the analgesic effect of acupuncture is mediated by adenosine A1 receptor activation at the acupuncture point, we here report that in acute and chronic animal pain models, oral intake of caffeine, a potent adenosine receptor antagonist, interferes with acupuncture analgesia, even at a low dose...
June 13, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28555252/the-perinatal-effects-of-maternal-caffeine-intake-on-fetal-and-neonatal-brain-levels-of-testosterone-estradiol-and-dihydrotestosterone-in-rats
#4
S Karaismailoglu, M Tuncer, S Bayrak, G Erdogan, E L Ergun, A Erdem
Testosterone, estradiol, and dihydrotestosterone are the main sex steroid hormones responsible for the organization and sexual differentiation of brain structures during early development. The hypothalamo-pituitary-adrenocortical axis, adrenal cells, and gonads play a key role in the production of sex steroids and express adenosine receptors. Caffeine is a non-selective adenosine antagonist; therefore, it can modulate metabolic pathways in these tissues. Besides, the proportion of pregnant women that consume caffeine is ∼60%...
May 29, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28547666/effects-of-caffeine-intake-prior-to-stress-cardiac-magnetic-resonance-perfusion-imaging-on-regadenoson-versus-adenosine-induced-hyperemia-as-measured-by-t1-mapping
#5
R van Dijk, D Kuijpers, T A M Kaandorp, P R M van Dijkman, R Vliegenthart, P van der Harst, M Oudkerk
The antagonistic effects of caffeine on adenosine receptors are a possible cause of false-negative stress perfusion imaging. The purpose of this study was to determine the effects of coffee intake <4 h prior to stress perfusion cardiac magnetic resonance imaging (CMR) in regadenoson- versus adenosine-induced hyperemia as measured with T1-mapping. 98 consecutive patients with suspected coronary artery disease referred for either adenosine or regadenoson perfusion CMR were included in this analysis. Twenty-four patients reported coffee consumption <4 h before CMR (15 patients with adenosine, and 9 patients with regadenoson); 74 patients reported no coffee intake (50 patients with adenosine, and 24 patients with regadenoson)...
May 25, 2017: International Journal of Cardiovascular Imaging
https://www.readbyqxmd.com/read/28546857/chloroquine-inhibits-ca-2-permeable-ion-channels-mediated-ca-2-signaling-in-primary-b-lymphocytes
#6
Yi-Fan Wu, Ping Zhao, Xi Luo, Jin-Chao Xu, Lu Xue, Qi Zhou, Mingrui Xiong, Jinhua Shen, Yong-Bo Peng, Meng-Fei Yu, Weiwei Chen, Liqun Ma, Qing-Hua Liu
BACKGROUND: Chloroquine, a bitter tastant, inhibits Ca(2+) signaling, resulting in suppression of B cell activation; however, the inhibitory mechanism remains unclear. RESULTS: In this study, thapsigargin (TG), but not caffeine, induced sustained intracellular Ca(2+) increases in mouse splenic primary B lymphocytes, which were markedly inhibited by chloroquine. Under Ca(2+)-free conditions, TG elicited transient Ca(2+) increases, which additionally elevated upon the restoration of 2 mM Ca(2+)...
2017: Cell & Bioscience
https://www.readbyqxmd.com/read/28530573/identification-of-a-key-umami-active-fraction-in-modernized-korean-soy-sauce-and-the-impact-thereof-on-bitter-masking
#7
Yiseul Kim, Eun-Young Kim, Hee Jin Son, Jai-Jung Lee, Yong-Ho Choi, Mee-Ra Rhyu
Food protein hydrolysates created by natural fermentation have been used for centuries as food flavorings. The aim of this study was to define the key umami-active fraction of modernized Korean soy sauce (mJGN) and the impact thereof on bitter-masking of human sensory and bitter-taste receptor-expressing cells. We found strong correlations between taste profiles of mJGN and a contained fraction (F05). The latter contained compounds of less than 500Da, and elicits a distinct umami taste. Both free amino acids and Glu-enriched oligopeptides are suggested to be crucial in terms of the effects of F05 on taste...
October 15, 2017: Food Chemistry
https://www.readbyqxmd.com/read/28525714/characterization-of-bitter-compounds-via-modulation-of-proton-secretion-in-human-gastric-parietal-cells-in-culture
#8
Kathrin I Liszt, Joachim Hans, Jakob P Ley, Elke Köck, Veronika Somoza
Humans perceive bitterness via around 25 different bitter receptors. Therefore, the identification of antagonists remains a complex challenge. We previously demonstrated several bitter tasting compounds such as caffeine to induce acid secretion in the stomach and in a human gastric tumor cell line (HGT-1). Here, the results of a fluorescent-based in vitro assay using HGT-1 cells and a human sensory panel testing nine selected potential bitter modulators with or without the bitter compounds caffeine or theobromine, were compared...
May 19, 2017: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/28524102/sleep-promoting-effects-and-possible-mechanisms-of-action-associated-with-a-standardized-rice-bran-supplement
#9
Hyejin Yang, Minseok Yoon, Min Young Um, Jaekwang Lee, Jonghoon Jung, Changho Lee, Yun-Tai Kim, Sangoh Kwon, Boknam Kim, Suengmok Cho
Natural sleep aids are becoming more popular due to the widespread occurrence of sleep disorders. The objective of this study was to assess the sleep-promoting effects of rice bran-a product that is considered as a functional ingredient. To evaluate the sleep-promoting effects of a standardized rice bran supplement (RBS), we employed a pentobarbital-induced sleep test and conducted analyses of sleep architecture. In addition, the effect of RBS on a caffeine-induced sleep disturbance was investigated. Oral administration of RBS (500 and 1000 mg/kg) produced a significant decrease in sleep latency and increase in sleep duration in pentobarbital-induced sleep in mice...
May 18, 2017: Nutrients
https://www.readbyqxmd.com/read/28513558/from-cell-to-beak-in-vitro-and-in-vivo-characterization-of-chicken-bitter-taste-thresholds
#10
Shira Cheled-Shoval, Maik Behrens, Ayelet Korb, Antonella Di Pizio, Wolfgang Meyerhof, Zehava Uni, Masha Y Niv
Bitter taste elicits an aversive reaction, and is believed to protect against consuming poisons. Bitter molecules are detected by the Tas2r family of G-protein-coupled receptors, with a species-dependent number of subtypes. Chickens demonstrate bitter taste sensitivity despite having only three bitter taste receptors-ggTas2r1, ggTas2r2 and ggTas2r7. This minimalistic bitter taste system in chickens was used to determine relationships between in-vitro (measured in heterologous systems) and in-vivo (behavioral) detection thresholds...
May 17, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28507584/effects-of-adenosine-receptor-antagonists-in-mptp-mouse-model-of-parkinson-s-disease-mitochondrial-dna-integrity
#11
Soha S Essawy, Mona Kamal Tawfik, Horya Erfan Korayem
INTRODUCTION: In Parkinson's disease (PD), compelling data indicate a functional link between adenosine/dopamine receptors and the progression of the neurodegenerative process. The present study was carried out to evaluate the effect of the non-selective adenosine receptor (ADR) antagonist caffeine, as well as the selective antagonists 8-cyclopentyl-1,3-dipropylxanthine (DPCPX), an ADRsA1 antagonist, and ((E)-1,3-diethyl-8-(3,4-dimethoxystyryl)-7-methyl-3,7-dihydro-1H-purine-2,6-dione) (KW-6002), an ADRsA2A antagonist, on the prevention of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-induced Parkinsonism in mice...
April 1, 2017: Archives of Medical Science: AMS
https://www.readbyqxmd.com/read/28485728/adenosine-a2a-receptor-inactivation-alleviates-early-onset-cognitive-dysfunction-after-traumatic-brain-injury-involving-an-inhibition-of-tau-hyperphosphorylation
#12
Z-A Zhao, Y Zhao, Y-L Ning, N Yang, Y Peng, P Li, X-Y Chen, D Liu, H Wang, X Chen, W Bai, J-F Chen, Y-G Zhou
Tau is a microtubule-associated protein, and the oligomeric and hyperphosphorylated forms of tau are increased significantly after neurotrauma and considered important factors in mediating cognitive dysfunction. Blockade of adenosine A2A receptors, either by caffeine or gene knockout (KO), alleviates cognitive dysfunction after traumatic brain injury (TBI). We postulated that A2AR activation exacerbates cognitive impairment via promoting tau hyperphosphorylation. Using a mouse model of moderate controlled cortical impact, we showed that TBI induced hyperphosphorylated tau (p-tau) in the hippocampal dentate gyrus and spatial memory deficiency in the Morris water maze test at 7 days and 4 weeks after TBI...
May 9, 2017: Translational Psychiatry
https://www.readbyqxmd.com/read/28476922/sarcolemmal-distribution-of-ica-and-incx-and-ca-autoregulation-in-mouse-ventricular-myocytes
#13
Hanne C Gadeberg, Cherrie H T Kong, Simon M Bryant, Andrew F James, Clive H Orchard
The balance of Ca influx and efflux regulates the Ca load of cardiac myocytes, a process known as autoregulation. Previous work has shown that Ca influx, via L-type Ca current (ICa), and efflux, via Na-Ca exchange (NCX), occur predominantly at t-tubules; however the role of t-tubules in autoregulation is unknown. We therefore investigated the sarcolemmal distribution of ICa and INCX, and autoregulation, in mouse ventricular myocytes using whole cell voltage-clamp and simultaneous Ca measurement in intact and detubulated (DT) cells...
May 5, 2017: American Journal of Physiology. Heart and Circulatory Physiology
https://www.readbyqxmd.com/read/28458351/caffeine-suppresses-the-activation-of-hepatic-stellate-cells-camp-independently-by-antagonizing-adenosine-receptors
#14
Momoka Yamaguchi, Shin-Ya Saito, Ryota Nishiyama, Misuzu Nakamura, Kenichiro Todoroki, Toshimasa Toyo'oka, Tomohisa Ishikawa
During liver injury, hepatic stellate cells (HSCs) are activated by various cytokines and transdifferentiated into myofibroblast-like activated HSCs, which produce collagen, a major source of liver fibrosis. Therefore, the suppression of HSC activation is regarded as a therapeutic target for liver fibrosis. Several epidemiological reports have revealed that caffeine intake decreases the risk of liver disease. In this study, therefore, we investigated the effect of caffeine on the activation of primary HSCs isolated from mice...
2017: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28444767/the-dual-orexin-receptor-antagonist-dora-22-lowers-histamine-levels-in-the-lateral-hypothalamus-and-prefrontal-cortex-without-lowering-hippocampal-acetylcholine
#15
Lihang Leon Yao, Andres Ramirez, Anthony J Roecker, Steven Fox, Jason Uslaner, Sean M Smith, Robert Hodgson, Paul J Coleman, John J Renger, Christopher J Winrow, Anthony L Gotter
Chronic insomnia is defined as a persistent difficulty with sleep initiation maintenance or non-restorative sleep. The therapeutic standard of care for this condition is treatment with gamma-aminobutyric acid (GABA)A receptor modulators, which promote sleep but are associated with a panoply of side effects, including cognitive and memory impairment. Dual orexin receptor antagonists (DORAs) have recently emerged as an alternative therapeutic approach that acts via a distinct and more selective wake-attenuating mechanism with the potential to be associated with milder side effects...
April 26, 2017: Journal of Neurochemistry
https://www.readbyqxmd.com/read/28430840/checkpoint-dependent-phosphorylation-of-med1-trap220-in-response-to-dna-damage
#16
Hyun-Ju Kim, Jeanho Yun
Mediator complex subunit 1 (Med1)/Thyroid hormone receptor-associated protein 220 (TRAP220), an essential component of thyroid hormone receptor-associated proteins (TRAP)/mediator, plays important roles in hormone responses and tumorigenesis. However, the role of Med1 in the DNA damage response has not been studied. In this study, we found that DNA damage, resulted from γ-irradiation, ultraviolet (UV)-irradiation, or hydroxyurea, induced phosphorylation of Med1 in vivo. Phosphorylation of Med1 was abrogated by either caffeine or wortmannin treatment, suggesting that Med1 is phosphorylated through the DNA damage checkpoint pathway...
June 1, 2017: Acta Biochimica et Biophysica Sinica
https://www.readbyqxmd.com/read/28420694/caffeine-preferentially-protects-against-oxygen-induced-retinopathy
#17
Shuya Zhang, Rong Zhou, Bo Li, Haiyan Li, Yanyan Wang, Xuejiao Gu, Lingyun Tang, Cun Wang, Dingjuan Zhong, Yuanyuan Ge, Yuqing Huo, Jing Lin, Xiao-Ling Liu, Jiang-Fan Chen
Retinopathy of prematurity (ROP) is the leading cause of childhood blindness, but current anti-VEGF therapy is concerned with delayed retinal vasculature, eye, and brain development of preterm infants. The clinical observation of reduced ROP severity in premature infants after caffeine treatment for apnea suggests that caffeine may protect against ROP. Here, we demonstrate that caffeine did not interfere with normal retinal vascularization development but selectively protected against oxygen-induced retinopathy (OIR) in mice...
April 18, 2017: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://www.readbyqxmd.com/read/28403410/assessing-the-pathogenicity-of-ryr1-variants-in-malignant-hyperthermia
#18
A Merritt, P Booms, M-A Shaw, D M Miller, C Daly, J G Bilmen, K M Stowell, P D Allen, D S Steele, P M Hopkins
Background: . Missense variants in the ryanodine receptor 1 gene ( RYR1 ) are associated with malignant hyperthermia but only a minority of these have met the criteria for use in predictive DNA diagnosis. We examined the utility of a simplified method of segregation analysis and a functional assay for determining the pathogenicity of recurrent RYR1 variants associated with malignant hyperthermia. Methods: . We identified previously uncharacterised RYR1 variants found in four or more malignant hyperthermia families and conducted simplified segregation analyses...
April 1, 2017: British Journal of Anaesthesia
https://www.readbyqxmd.com/read/28390800/ca-2-release-via-two-pore-channel-type-2-tpc2-is-required-for-slow-muscle-cell-myofibrillogenesis-and-myotomal-patterning-in-intact-zebrafish-embryos
#19
Jeffrey J Kelu, Sarah E Webb, John Parrington, Antony Galione, Andrew L Miller
We recently demonstrated a critical role for two-pore channel type 2 (TPC2)-mediated Ca(2+) release during the differentiation of slow (skeletal) muscle cells (SMC) in intact zebrafish embryos, via the introduction of a translational-blocking morpholino antisense oligonucleotide (MO). Here, we extend our study and demonstrate that knockdown of TPC2 with a non-overlapping splice-blocking MO, knockout of TPC2 (via the generation of a tpcn2(dhkz1a) mutant line of zebrafish using CRISPR/Cas9 gene-editing), or the pharmacological inhibition of TPC2 action with bafilomycin A1 or trans-ned-19, also lead to a significant attenuation of SMC differentiation, characterized by a disruption of SMC myofibrillogenesis and gross morphological changes in the trunk musculature...
April 6, 2017: Developmental Biology
https://www.readbyqxmd.com/read/28387457/dampened-activity-of-ryanodine-receptor-channels-in-mutant-skeletal-muscle-lacking-tric-a
#20
Sam El-Ajouz, Elisa Venturi, Katja Witschas, Matthew Beech, Abigail D Wilson, Chris Lindsay, David Eberhardt, Fiona O'Brien, Tsunaki Iida, Miyuki Nishi, Hiroshi Takeshima, Rebecca Sitsapesan
KEY POINTS: The role of trimeric intracellular cation (TRIC) channels is not known, although evidence suggests they may regulate ryanodine receptors (RyR) via multiple mechanisms. We therefore investigated whether Tric-a gene knockout (KO) alters the single-channel function of skeletal RyR (RyR1). We find that RyR1 from Tric-a KO mice are more sensitive to inhibition by divalent cations, although they respond normally to cytosolic Ca(2+) , ATP, caffeine and luminal Ca(2+) . In the presence of Mg(2+) , ATP cannot effectively activate RyR1 from Tric-a KO mice...
April 7, 2017: Journal of Physiology
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